反应详情

温度

120 °C

2-(4-tert-Butoxycarbonylamino-benzoylamino)-3-[3-fluoro-4-(N-hydroxycarbamimidoyl)-phenyl]-propionic acid ethyl ester. A mixture of 2-(4-tert-butoxycarbonylamino-benzoylamino)-3-(4-cyano-3-fluoro-phenyl)-propionic acid ethyl ester (214 mg, 0.47 mmol), NH2OH.HCl (49 mg 0.71 mmol), and NaHCO3 (79 mg, 0.94 mmol) in EtOH (10 mL) was heated under microwave at 120° C. for 20 min and then allowed to cool to room temperature. The mixture was filtered, concentrated in vacuo, and purified by silica gel chromatography to give the title compound (170 mg) as a white solid.

1. temperatureto cool to room temperature
2. filtrationThe mixture was filtered
3. concentrationconcentrated in vacuo
4. custompurified by silica gel chromatography